Abstract: A method for inhibiting the growth of a microorganism using an effective amount of one or more of the following synthetic brominated furanones: (i) 4-bromo-5Z-(bromomethylene)-3-methylfuran-2-one; (ii) 3-(dibromomethyl)-5-(dibromomethylene)furan-2-one; (iii) 3-(bromomethyl)-5-(dibromomethylene)furan-2-one; (iv) 4-bromo-3-(bromomethyl)-5Z-(bromomethylene)furan-2-one; or (v) 4-bromo-5-(dibromomethyl)-3-methylfuran-2(5H)-one. The brominated furanones inhibit the growth of both fungi and bacteria, including the fungal species Candida albicans, Gloeophyllum trabeum, Chaetomium globosum, and Trametes versicolor and the bacterial species Pseudomonas aeruginosa. The brominated furanones can be used topically or internally to treat human infections, and can be used to treat other objects, such as wood building supplies, to prevent fungal rot.

Abstract: The present invention relates to lactone compounds represented by the following Formulas I and II, and methods of making such lactone compounds. The present invention also relates to methods of making other materials from such lactone compounds, such as fused ring indenol compounds (e.g., indeno-fused naphthols), and fused ring indenopyran compounds (e.g., indeno-fused naphthopyrans).

Abstract: The present invention relates to a process of the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one of the formula by employing a dialkylmalonate of the formula wherein R1b is lower alkyl, and the use of this process for the manufacture of DPP-IV inhibitors that are useful for the treatment and/or prophylaxis of diseases such as diabetes.

Abstract: This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.

Abstract: A 5-methylene-1,3-dioxolan-4-one derivative and a monomer and copolymer thereof and a resist composition containing the polymer or copolymer where the 5-methylene-1,3 -dioxolan-4-one derivative is of formula (1): wherein R1 represents a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms, or a linear or branched alkyl group containing 1 to 6 carbon atoms which has a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms as a substituent; R2 represents a hydrogen atom, or a linear or branched alkyl group containing 1 to 6 carbon atoms; or R1 and R2 represent a bridged cyclic hydrocarbon group containing 4 to 16 carbon atoms together with the carbon atom to which they are bound, provided that the alkyl group and the bridged cyclic hydrocarbon group may have at least one substituent selected from a group consisting of a linear or branched alkyl group containing 1 to 6 carbon atoms which may be optionally substituted, a hydroxy group, a carboxy group, an acyl group containing 2 to 6 car

Abstract: The invention relates to chiral nonracemic liquid crystal compounds having achiral tails comprising a perfluoroalkyl terminal portion which are useful as components in liquid crystal to impart high polarization to the mixture. The materials of this invention can be combined with known liquid crystal host materials to impart improved properties. Chiral nonracemic compounds of this invention can function as additives or dopants in host materials to impart chirality into an LC material.

Abstract: A process for preparing functionalized ?-butyrolactones 3 and various biologically active compounds using mucohalic acid 1 and halide 2 in the presence of indium is disclosed, wherein X, Y, R1, R2, and R3 may have any of the meanings defined herein

Abstract: A method for the preparation of a compound of formula (II) wherein R1 and R2 are independently H, alkyl, alkoxy, oxoalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optionally interrupted by one or more hetero atoms, straight chain or branched chain, hydrophilic, hydrophobic or fluorophilic; R3, R4, R5 and R6 are independently or all hydrogen or halogen; provided that at least two of the R3, R4, R5 and R6 are halogens.

Abstract: A process for preparing functionalized &ggr;-butyrolactones 3 and various biologically active compounds using mucohalic acid 1 and halide 2 in the presence of indium is disclosed, wherein X, Y, R1, R2, and R3 may have any of the meanings defined herein.

Abstract: The invention provides new methods for preparation of cyclic oxygen compounds, including 2,5-disubstituted tetrahydrofurans, 2,6-disubstituted tetrahydropyrans, 2,7-disubstituted oxepanes and 2,8-oxocanes. The invention also provides new cyclic oxygen compounds and pharmaceutical compositions and therapeutic methods that comprise such compounds.

Abstract: Process for producing butyrolactones of the general formula I where R1 and R2 are each hydrogen, alkyl, hydroxyalkyl, substituted or unsubstituted aryl or substituted or unsubstituted trialkylsilyl, by reacting alkynes of the general formula II where R1 and R2 are each as defined above, with carbon monoxide and water in the presence of a rhodium catalyst under pressures from 20 to 300 bar and hydrogenating the unhydrogenated 2(5H)-furanone intermediates comprises a) reacting the carbonylation reaction mixture with hydrogen at from 150 to 250° C. and from 100 to 300 bar, b) removing the precipitated catalyst and returning it into the carbonylation reaction, and c) subjecting the catalyst-free reaction mixture to a distillation to recover the butyrolactone.

Abstract: Fluorine-containing, chiral liquid crystal compounds comprise (a) a chiral fluorochemical terminal portion comprising (i) at least one chiral center, which can optionally be heteroatom-substituted; (ii) a terminal fluoroalkyl, fluoroether, perfluoroalkyl, or perfluoroether group; and (iii) an alkylene or fluoroalkylene group optionally containing at least one catenary ether oxygen atom; (b) a chiral or achiral terminal portion consisting of a hydrocarbon or hydrocarbon ether group, and, when chiral, comprising at least one chiral center, which can optionally be heteroatom-substituted; and (c) a central core connecting the terminal portions; the alkylene or fluoroalkylene group of the chiral fluorochemical terminal portion having at least 3 in-chain atoms and being located between the chiral center of the chiral fluorochemical terminal portion and the central core. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.

Abstract: Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the .alpha.-hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the .alpha.-hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.

Abstract: The invention provides substituted furanone antiarthritic and analgesic pharmaceutical agents defined by Formula I, ##STR1## wherein: R.sup.1 is selected from the group consisting of(a) S(O).sub.2 CH.sub.3,(b) S(O).sub.2 NH.sub.2,(c) S(O).sub.2 NHC(O)CF.sub.3,(d) S(O)(NH)CH.sub.3,(e) S(O)(NH)NH.sub.2,(f) S(O)(NH)NHC(O)CF.sub.3,(g) P(O)(CH.sub.3)OH, and(h) P(O)(CH.sub.3)NH.sub.2 ;R.sup.2 and R.sup.3 independently are selected from(1) hydrogen,(2) halo,(3) C.sub.1 -C.sub.6 alkyl,(4) C.sub.1 -C.sub.6 alkoxy, and(5) C.sub.1 -C.sub.6 alkylthio;n is an integer from 1 to 3;m is an integor from 1 to 3;or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides novel haloenol lactones that are effective as active site inhibitors of cholesterol esterase. By inhibiting cholesterol esterase the inhibitors of the present invention provide a new approach to the treatment of hypercholesterolemia through limiting the bioavailability of dietary cholesterol.

Abstract: Fluorine-containing, chiral liquid crystal compounds comprise (a) a chiral fluorochemical terminal portion comprising (i) at least one chiral center, which can optionally be heteroatom-substituted; (ii) a terminal fluoroalkyl, fluoroether, perfluoroalkyl, or perfluoroether group; and (iii) an alkylene or fluoroalkylene group optionally containing at least one caternary ether oxygen atom; (b) a chiral or achiral terminal portion consisting of a hydrocarbon or hydrocarbon ether group, and, when chiral, comprising at least one chiral center, which can optionally be heteroatom-substituted; and (c) a central core connecting the terminal portions; the alkylene or fluoroalkylene group of the chiral fluorochemical terminal portion having at least 3 in-chain atoms and being located between the chiral center of the chiral fluorochemical terminal portion and the central core. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.

Abstract: There are described N-aminopyridone derivatives of the formula I: ##STR1## where the substituents R.sup.1 to R.sup.12 have the meanings given in claim 1, a process for their preparation, and their use for controlling undesirable vegetation.

Abstract: Novel nonpeptide antagonists of endothelin (I) are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prostatic hyperplasia (BPH), and diabetes.

Abstract: A vitamin D.sub.3 derivative represented by the following formula: wherein, R is, independently, a hydrogen atom, tri(C.sub.1 to C.sub.7 hydrocarbon)silyl group, C.sub.2 to C.sub.8 acyl group, or group forming an acetal bond together with an oxygen atom of a hydroxyl group, A is ##STR1## where, R.sup.1 is a methyl group or methylene group, and when R.sup.1 is a methylene group, the bond between the R.sup.1 and the 3-position of the lactone ring is a double bond, R.sup.2 is a hydrogen atom or C.sub.1 to C.sub.3 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together indicate a substitutable single methylene group.

Abstract: A compound of formula I, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' are independently the same or different and each represent hydrogen, hydroxy, or lower alkoxy, or any vicinal two of R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' combined together represent --O--(CH.sub.2).sub.n --O--, wherein n=1 or 2; R.sub.4 represents methylene or halomethyl; and X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are independently the same or different and each represent hydrogen or halogen; or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition that contains an effective amount of a compound of formula I together with a pharmaceutically acceptable excipient, and a method of treating cancer that involves the administration of an effective amount of the compound of formula I to a patient in need thereof.

Abstract: Fluorine-containing, chiral liquid crystal compounds comprise (a) a chiral fluorochemical terminal portion containing at least one methylene group and optionally containing at least one catenary ether oxygen atom; (b) a saturated, chiral or achiral, hydrocarbon terminal portion; and (c) a central core connecting the terminal portions. The compounds have smectic mesophases or latent smectic mesophases and are useful, for example, in liquid crystal display devices.

Abstract: An optically active compound represented by the formula R.sub.1 --A.sub.1 --A.sub.2 --X.sub.1 --A.sub.3 --(CH.sub.2).sub.p --L--A.sub.4 --R.sub.2, in which R.sub.1 is F, CN or straight chain, branched or cyclic alkyl and R.sub.2 is H, F, CH or straight chain or branched alkyl; A.sub.3 is 1,4-phenylene, pyridine-2,5-diyl, pyrimidine-2,5-diyl, pyrazine-2,5-diyl, pyridazine-3,6-diyl, 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, 1,3-ditiane-2,5-diyl, thiophene-2,5-diyl, thiazole-2,5-diyl, thiaziazole-2,5-diyl, benzoxazole-2,5-diyl, benzoxazole-2,6-diyl, benzothiazole-2,5-diyl, benzothiazole-2,6-diyl, benzofuran-2,5-diyl, benzofuran-2,6-diyl, quinoxaline-2,6-diyl, quinoline-2,6-diyl, 2,6-naphthylene, indane-2,5-diyl, 2-alkylindane-2,5-diyl, indanone-2,6-diyl, 2-alkylindane-2,6-diyl, coumarane-2,5-diyl and 2-alkylcoumarane-2,5-diyl; A.sub.1, A.sub.2 and A.sub.4 are single bond or A.sub.3 ; X.sub.1 ' is a single bond, --COO--, --OCO--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.

Abstract: The present invention relates to a process for producing lactones starting from cyclic ketones which comprises an oxidation reaction which is performed in the presence of an optionally substituted cycloaliphatic peracid or of an optionally substituted aliphatic peracid that is immiscible with water. The process allows to obtain high selectivity, does not entail the use of dangerous reagents, and allows excellent economic advantages.

Abstract: 5-Oxaspiro[2.4]heptan-6-one: ##STR1## is obtained from [3-(hydroxymethyl)oxetan-3-yl]acetonitrile by reaction with hydrogen bromide and then cyclizing the intermediate product 4,4-bis(bromomethyl)dihydro-2-furanone with zinc. 5-Oxaspiro[2.4]heptan-6-one is an intermediate product for the production of leukotriene antagonists.

Abstract: A process for preparing 5-membered ring heterocycles of the general formula I ##STR1## where R.sup.1 is methyl or hydroxyethyl,R.sup.2,R.sup.3,R.sup.4,R.sup.5 and R.sup.6 are hydrogen, C.sub.1 - to C.sub.12 -alkyl, C.sub.2 - to C.sub.12 -alkenyl, aryl, C.sub.3 - to C.sub.8 -cycloalkyl, C.sub.1 - to C.sub.12 -alkoxy, halogen, C.sub.2 - to C.sub.20 -alkoxycarbonylalkyl, C.sub.2 - to C.sub.20 -alkylcarbonyloxy, formyl, C.sub.2 - to C.sub.20 -formylalkyl, benzoyl or --CH(OR.sup.3)(OR.sup.5), or R.sup.3 and R.sup.5 together are a C.sub.2 - to C.sub.7 -alkylene chain which is unsubstituted or monosubstituted to pentasubstituted by R.sup.4 or a .dbd.CH--CH.dbd.CH--CH.dbd. unit which is unsubstituted or monosubstituted to tetrasubstituted by R.sup.4,X is oxygen or N--R.sup.4by reacting 5-membered ring heterocycles of the general formula II ##STR2## where R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the abovementioned meanings and Y is hydrogen, acetyl or C.sub.2 - to C.sub.

Abstract: Compounds based on 3,4-diaryl-(5H)-furan-2-one, with fungicidal activity, having the general formula (I): ##STR1##

Abstract: A process for simultaneously producing a lactone and an aromatic carboxylic acid, which comprises oxidizing a cyclic ketone and an aromatic aldehyde wherein: the cyclic ketone/aromatic aldehyde molar ratio is set at 1.1:1 to 20:1 and the throughput of the aromatic aldehyde per a unit reaction solution volume and a unit time is set at 0.05 to 1.5 mol/1.hour.

Abstract: The invention provides a novel process for the manufacture of enantiomerically-pure halolactones of the formula I which are useful for the production of certain 5-amino-4-hydroxyvaleric acid derivatives, themselves valuable intermediates in the production of compounds which are renin inhibitors. The process involves a diastereoselective alkylation of an oxazolidinone of the formula III, followed by a highly stereoselective and novel halolactonisation of an oxazolidinone of the formula II. Certain of the oxazolidinones of the formula II are novel and are provided as a further feature of the invention. The invention also provides a novel process for the production of the pharmaceutically-useful 5-amino-4-hydroxyvaleric acid derivatives of formula VI.

Abstract: Variously substituted 4-(biphen-2-ylmethylcarbamoyl)-3-hydroxybutyric acids and esters, also named as N-(biphen-2-yl)-3-hydroxyglutaramic acid derivatives, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.

Abstract: A process for recycling the difluoro sugar in the synthesis of 2,2-difluoronucleosides proceeds by removing the base moiety of .alpha.-difluoronucleosides by reduction and hydrolysis, followed by oxidation to put the difluro sugar in a form conventiently recycled into the synthesis, and intermediates useful therefor.

Abstract: A process for preparing 5-substituted-3-furaldehydes which comprises reacting 3-furaldehyde with lithium morpholide, followed by sec-butyl lithium, followed by an electrophile.

Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.

Abstract: A process for the preparation of perfluoroalkylated ketones and/or perfluoroalkylated alcohols, comprising the step of contacting a perfluoroalkyl iodide or perfluoroalkyl bromide with an acid anhydride, in the presence of a metal chosen from zinc and cadmium.

Abstract: .gamma.-butyrolactones of the general formula I ##STR1## where R.sup.1 is hydrogen or alkyl of 1 to 4 carbon atoms which may be substituted by lower alkoxy or acyloxy and R.sup.2 is hydrogen or straight-chain or branched alkyl which is unsubstituted or substituted by a functional group or is aryl, are prepared by reacting an alkylene oxide of the general formula II ##STR2## with an acylacetate of the general formla III ##STR3## where R.sup.1 and R.sup.2 have the above meanings and R.sup.3 and R.sup.4 are each alkyl of 1 to 6 carbon atoms or aryl, and R.sup.4 may furthermore be hydrogen, in the presence of a catalyst at elevated temperatures, by a process in which the reaction is carried out in the presence of an alkali metal halide, of an ammonium halide, preferably a quaternary ammonium halide, of a phosphonium halide, of an alkali metal phosphate or of an alkali metal carbonate at from 20.degree. to 200.degree. C. and under from 1 to 50 bar.

Abstract: A novel three-step process for preparing 4-(3,4-dichlorophenyl)-4-phenylbutanoic acid is disclosed, which involves (1) reducing 4-(3,4-dichlorophenyl)-4-ketobutanoic acid to 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid; (2) then converting the intermediate hydroxy acid formed in the first step to 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone, and (3) thereafter reacting the resulting gamma-butyrolactone compound with benzene in a Friedel-Crafts type reaction to form the desired final product. The latter compound is known to be useful as an intermediate leading to cis-(1S)(4S)- -N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine (sertraline), which is known to be a preferred anti-depressant agent in the field of medicinal chemistry. The aforementioned 5-(3,4-dichlorophenyl)-dihydro-2(3H)-furanone and 4-(3,4-dichlorophenyl)-4-hydroxybutanoic acid are both novel compounds.

Abstract: Polyfluoro .gamma.-ketoester compounds are obtained by reaction of ethylenic monoolefins, a metal or quaternary ammonium cyanide, and a fluoroester. These compounds, which have a general formula R.sub.F C(O)CFYCF.sub.2 CO.sub.2 R.sup.1, can be copolymerized directly with fluorinated ethylenic monoolefins, or further reacted to form vinyl ether and allyl ether derivatives which may also be copolymerized with ethylenic comonomers, forming solid, moldable copolymers with useful properties determined by the nature of pendant functional groups R.sub.F.

Abstract: The following process steps are shown: ##STR1## Intermediates I, II, and VI are new. End product IV is a known intermediate in the preparation of known pyrethroid-like cyclopropanecarboxylic acid ester insecticides.

Abstract: There are disclosed substituted lactones of the formula ##STR1## wherein A stands for --CH--CH.sub.2 X (X being Cl, Br or OH), --CHY--CHY-- (Y being Cl or Br), or ##STR2## and R.sup.1, R.sup.2 and R.sup.3 are the same or different radicals from the group of hydrogen and C.sub.1 to C.sub.10 alkyls, at least one of the radicals R.sup.2, R.sup.2 and R.sup.3 being such an alkyl radical, and process for making the same.

Abstract: Novel .gamma.-lactone derivatives are provided. These lactone derivatives, when reacted with hydrogen halide in alcohol, yield .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters. This ring-opening process is useful for the purpose of increasing the yield of pyrethrin analogs which are of value as insecticides and agricultural chemicals. Thus, the .gamma.-lactone derivatives by-produced in the production process for dihalogenovinyl chrysanthemumates are caused to undergo ring-opening reaction to yield the corresponding .gamma.-halogeno-.delta.-unsaturated carboxylic acid esters which are important intermediates for said pyrethrin analogs.

Abstract: A method for the synthesis of lepiochlorin, an antibiotic.

Abstract: This invention relates to 2-aryl-2-1-H-azoyl-(alkyl)gamma-butyrolactone of the formula: ##STR1## wherein Z is optionally substituted aryl;R is hydrogen, alkyl, alkenyl, alkynyl, optionally substituted aryl or optionally substituted aralkyl;Azo is 1-H-imidiazoyl, 1-H-1,2,4-triazoyl or 4-H-1,2,4-triazoyl;n is zero or an integer from 1 to 5, and the agronomically acceptable acid addition salts and metal salt complexes thereof, methods for their preparation and their use as pesticides.

Abstract: There are disclosed substituted lactones of the formula ##STR1## wherein A stands for --CH--CH.sub.2 X (X being Cl, Br or OH), --CHY--CHY-- (Y being Cl or Br), or ##STR2## and R.sup.1, R.sup.2 and R.sup.3 are the same or different radicals from the group of hydrogen and C.sub.1 to C.sub.10 alkyls, at least one of the radicals R.sup.1, R.sup.2 and R.sup.3 being such an alkyl radical, and process for making the same.